Design, synthesis and pharmacological evaluation of N3 aryl/ heteroaryl substituted 2-((benzyloxy and phenylthio) methyl) 6,7- dimethoxyquinazolin-4(3H)-ones as potential anticonvulsant agents

• Published in: Medicinal chemistry (Shp-sariqah, United Arab Emirates) Vol. 10; no. 8; p. 800
• Main Authors: Das, Nirupam, Banerjee, Anupam G, Shrivastava, Sushant K
• Format: Journal Article
• Language: English
• Published: Netherlands 01.01.2014
• Subjects: Alanine Transaminase - blood; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid - administration & dosage; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid - adverse effects; Animals; Anticonvulsants - chemical synthesis; Anticonvulsants - chemistry; Anticonvulsants - pharmacology; Aspartate Aminotransferases - blood; Convulsants - administration & dosage; Disease Models, Animal; Drug Design; Drug Evaluation, Preclinical; Electroshock; Female; Injections, Intraventricular; Injections, Subcutaneous; Liver - drug effects; Liver - pathology; Male; Mice; Motor Activity - drug effects; Pentylenetetrazole - administration & dosage; Quinazolinones - chemical synthesis; Quinazolinones - chemistry; Quinazolinones - pharmacology; Rats; Rotarod Performance Test; Seizures - blood; Seizures - chemically induced; Seizures - drug therapy; Seizures - physiopathology; Structure-Activity Relationship

Novel N3 aryl/heteroaryl substituted 2-((benzyloxy and phenylthio) methyl) 6,7-dimethoxyquinazolin-4(3H)- ones (8a-8l) were synthesized and evaluated for their anticonvulsant activity using various models of epilepsy, such as maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) and in...